PIK75

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PIK-75 Hydrochronide 是一种 p110α 抑制剂，IC50 为 5.8 nM（比 p110β 强 200 倍），是 Ser773 的异构体特异性突变体，并且还能有效抑制 DNA-PK，在无细胞测定中 IC50 为 2 nM。

PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.

PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC50s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively.PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC50 values of 1.2 and 1.3 μM, respectively. PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC50 of 78 nM.PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death.PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells. Cell Viability Assay Cell Line:Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1) Concentration:0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM Incubation Time:48 hours Result:Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment.Western Blot Analysis Cell Line:Overnight-starved CHO-IR cells Concentration:1, 10, 100, 1000 nM Incubation Time:5 minutes Result:Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner.PIK-75 potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice.

PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice. Animal Model:Mice bearing tumors of MIA PaCa-2 Dosage:2 mg/kg; or combination with Gemcitabine (20 mg/kg) Administration:Administered injection; 5 times per week. 25 days Result:Reduced the tumor growth and enhanced the antitumor effect.

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Metabolic Enzyme/Protease

P450

DNA-PK| p110α| p110β| p110γ| p110δ

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372196-67-3

452.28

C16H14BrN5O4S

>98% (HPLC)

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CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)/N=C/C2=CN=C3N2C=C(C=C3)Br

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(-20℃)

With Ice Pack

≥ 2 years